Abstract
The aim of this study was to clarify the anti-inflammatory mechanism of apigenin. Apigenin inhibited the collagenase activity involved in rheumatoid arthritis (RA) and suppressed lipopolysaccharide (LPS)-induced nitric oxide (NO) production in a dose dependent manner in RAW 264.7 macrophage cells. Pretreatment with apigenin also attenuated LPS-induced cyclooxygenase-2 (COX-2) expression. In addition, apigenin profoundly reduced the tumor necrosis factor-alpha (TNF-alpha)-induced adhesion of monocytes to HUVEC monolayer. Apigenin significantly suppressed the TNF-alpha-stimulated upregulation of vascular cellular adhesion molecule-1 (VCAM-1)-, intracellular adhesion molecule-1 (ICAM-1)-, and E-selectin-mRNA to the basal levels. Taken together, these results suggest that apigenin has significant anti-inflammatory activity that involves blocking NO-mediated COX-2 expression and monocyte adherence. These results further suggest that apigenin may be useful for therapeutic management of inflammatory diseases.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antioxidants / pharmacology
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Apigenin / pharmacology*
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Cell Adhesion / drug effects*
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Cell Adhesion Molecules / genetics
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Cell Adhesion Molecules / metabolism*
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Cell Line
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Cells, Cultured
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Collagenases / metabolism
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Cyclooxygenase 2 / metabolism*
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Cyclooxygenase 2 Inhibitors / pharmacology*
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Dose-Response Relationship, Drug
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E-Selectin / metabolism
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Endothelial Cells / drug effects*
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Endothelial Cells / metabolism
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Humans
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Hyaluronoglucosaminidase / antagonists & inhibitors
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Hyaluronoglucosaminidase / metabolism
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Intercellular Adhesion Molecule-1 / metabolism
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Lipopolysaccharides / pharmacology
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Macrophages / drug effects*
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Macrophages / enzymology
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Macrophages / metabolism
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Matrix Metalloproteinase Inhibitors
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Mice
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Monocytes / drug effects*
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Monocytes / metabolism
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Nitric Oxide / metabolism
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RNA, Messenger / metabolism
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Tumor Necrosis Factor-alpha / metabolism
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Umbilical Veins / drug effects
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Umbilical Veins / metabolism
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Vascular Cell Adhesion Molecule-1 / metabolism
Substances
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Antioxidants
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Cell Adhesion Molecules
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Cyclooxygenase 2 Inhibitors
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E-Selectin
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Lipopolysaccharides
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Matrix Metalloproteinase Inhibitors
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RNA, Messenger
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Tumor Necrosis Factor-alpha
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Vascular Cell Adhesion Molecule-1
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Intercellular Adhesion Molecule-1
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Nitric Oxide
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Apigenin
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Ptgs2 protein, mouse
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Cyclooxygenase 2
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Hyaluronoglucosaminidase
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Collagenases